2. Academic Validation
  3. Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD)

Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD)

  • Bioorg Med Chem Lett. 2022 Jun 15;66:128734. doi: 10.1016/j.bmcl.2022.128734.
Jianyu Lu 1,  Chi-Chung Chan 2,  Deheng Sun 2,  Guoping Hu 2,  Huijun He 1,  Jian Li 2,  Jiaqiang Dong 3,  Kai Liu 3,  Liang Shen 2,  Lihong Hu 1,  Qingyang Gu 2,  Shuhui Chen 2,  Tielin Wang 3,  Ting Gong 3,  Wei Tang 3,  Xiaoting Li 1,  Xiaotong Zhu 3,  Xu Zeng 1,  Yingjie Zhu 2,  Yuanfeng Xia 2,  Yuanyuan Huang 2,  Yusong Zhu 2,  Zhenteng Liu 3,  Charles Z Ding 4
Affiliations

Affiliations

  • 1 WuXi AppTec, 666 Gaoxin Road, East Lake High-tech Development Zone, Wuhan 430075, China.
  • 2 WuXi AppTec, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China.
  • 3 Luoxin Pharmaceutical (Shanghai) Co., Ltd., Building 1 and 1st-3rd Floors, Building 2, No.85 Faladi Road, China (Shanghai) Pilot Free Trade Zone, Shanghai 201210, China.
  • 4 WuXi AppTec, 288 Fute Zhong Road, Waigaoqiao Free Trade Zone, Shanghai 200131, China. Electronic address: charles_ding@wuxiapptec.com.
PMID: 35436589 DOI: 10.1016/j.bmcl.2022.128734
Abstract

We previously described the discovery of a novel indole series compounds as oral SERD for ER positive breast Cancer treatment. Further SAR exploration focusing on substitutions on indole moiety of compound 12 led to the discovery of a clinical candidate LX-039. We report herein its profound anti-tumor activity, desirable ER antagonistic characteristics combined with favorable pharmacokinetic and preliminary safety properties. LX-039 is currently in clinical trial (NCT04097756).

Keywords

Estrogen receptor; Indole; SERD.

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